STAT3-IN-1 |
Catalog No.GC37688
One-Click Copy Product Info
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STAT3-IN-1 is a potent, selective, and orally active inhibitor of STAT3 with IC50 values of 1.82μM and 2.14μM in HT29 and MDA-MB-231 cells, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2059952-75-7
Sample solution is provided at 25 µL, 10mM.
STAT3-IN-1 is a potent, selective, and orally active inhibitor of STAT3 with IC50 values of 1.82μM and 2.14μM in HT29 and MDA-MB-231 cells, respectively [1]. STAT3-IN-1 inhibits both STAT3 acetylation and phosphorylation, leading to increased NKG2D ligand expression and decreased IL-10 levels[1-2]. STAT3-IN-1 has been widely used to induce growth arrest and tumor cell death in Meta4 organoids[3].
In vitro, STAT3-IN-1 treatment at 1μM for 8h significantly inhibited the decrease in Nos2 mRNA levels and the increase in IL-1β and IL-6 levels caused by 100μg/ml zymosan in mouse primary bone marrow dendritic cells (BMDCs)[4]. STAT3-IN-1 treatment (3μM) for 48h suppressed the cell migration of DU145 cells induced by CCL5 and retarded the upregulation of Snail and TWIST[5].
In vivo, STAT3-IN-1 treatment via oral administration at a dose of 20mg/kg daily for 14 days significantly inhibited tumor growth in a xenograft model of 4T1 cells without affecting body weight[6]. Injecting STAT3-IN-1 (5mg/kg) and temozolomide (5mg/kg) intratumorally every 5 days for 10 consecutive days can significantly inhibit the tumor growth of A375 cell-xenograft mice with overexpressed RPL18 and improve the survival rate[7].
References:
[1] Hu Y, Dong Z, Liu K. Unraveling the complexity of STAT3 in cancer: molecular understanding and drug discovery[J]. Journal of Experimental & Clinical Cancer Research, 2024, 43(1): 23.
[2] Jia Z, Xiao B, Li J, et al. BTK inhibitors enhance NKG2D ligand expression by regulating IL-10/STAT3 pathway in activated non-GCB diffuse large B-cell lymphoma cells[J]. Anti-Cancer Drugs, 2025, 36(5): 374-382.
[3] Kim H, Jang B, Zhang C, et al. Targeting stem cells and dysplastic features with dual MEK/ERK and STAT3 suppression in gastric carcinogenesis[J]. Gastroenterology, 2024, 166(1): 117-131.
[4] Wu H, Yin X, Zhao X, et al. HDAC11 negatively regulates antifungal immunity by inhibiting Nos2 expression via binding with transcriptional repressor STAT3[J]. Redox Biology, 2022, 56: 102461.
[5] Ma J, Shayiti F, Ma J, et al. Tumor‐associated macrophage‐derived CCL5 promotes chemotherapy resistance and metastasis in prostatic cancer[J]. Cell biology international, 2021, 45(10): 2054-2062.
[6] Li S, Zhang W, Yang Y, et al. Discovery of oral-available resveratrol-caffeic acid based hybrids inhibiting acetylated and phosphorylated STAT3 protein[J]. European journal of medicinal chemistry, 2016, 124: 1006-1018.
[7] Zuo C, Hu C, Jiang X, et al. RPL18 promotes melanoma progression and drug resistance via BTF3/STAT3-dependent mechanisms and immune modulation[J]. iScience, 2026, 29(1).
| Cell experiment [1]: | |
Cell lines | DU145 cells |
Preparation Method | DU145 cells were cultured in RPMI 1640 medium containing 10% fetal bovine serum (FBS) at 37℃ in the presence of 5% CO2. Cells migrating assay was detected using 8-μm trans-well chambers. DU145 cells were pretreated with STAT3-IN-1 (3μM) and CCL5 (100ng/ml) for 48h. 5×104 cells in 150μl non-serum culture medium were seeded into the upper chambers. A total of 800μl culture medium containing 10% FBS medium was added into the lower chambers. Twenty-four hours later, trans-wells were washed with phosphate-buffered saline (PBS), fixed with formalin, and stained with 0.1% crystal violet. Cells were counted in three random fields per well under a ×100 microscope. |
Reaction Conditions | 3μM; 48h |
Applications | STAT3-IN-1 treatment suppressed the cell migration of DU145 cells induced by CCL5. |
| Animal experiment [2]: | |
Animal models | Female Kunming mice |
Preparation Method | Adult female Kunming mice (4-6 weeks of age) were group-housed in polysulfone cages with bedding material, and were housed in a room with controlled humidity (50±10%) and temperature (25±3°C) under a 12/12h light/dark cycle. All mice were adaptively fed for one week. Freshly harvested breast cancer cells 4T1 (2.5×106 cells per mouse, resuspended in 100μl PBS) were injected into the armpit of the mice. The mice were given 20mg/kg STAT3-IN-1, or vehicle p.o. once daily. Body weights were measured every other day. On the 14th day, all mice were killed, and the tumor was segregated and weighed. |
Dosage form | 20mg/kg/day for 14 days; p.o. |
Applications | STAT3-IN-1 treatment inhibited tumor growth in a xenograft model of 4T1 cells without affecting body weight. |
References: | |
| Cas No. | 2059952-75-7 | SDF | |
| Canonical SMILES | COC1=CC(OC)=CC(/C=C/C2=CC=C(NC(/C=C/C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=C1 | ||
| Formula | C28H29NO6 | M.Wt | 475.53 |
| Solubility | DMSO: 125 mg/mL (262.86 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1029 mL | 10.5146 mL | 21.0292 mL |
| 5 mM | 420.6 μL | 2.1029 mL | 4.2058 mL |
| 10 mM | 210.3 μL | 1.0515 mL | 2.1029 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)